AU2013204727A1 - Therapeutic compounds - Google Patents
Therapeutic compounds Download PDFInfo
- Publication number
- AU2013204727A1 AU2013204727A1 AU2013204727A AU2013204727A AU2013204727A1 AU 2013204727 A1 AU2013204727 A1 AU 2013204727A1 AU 2013204727 A AU2013204727 A AU 2013204727A AU 2013204727 A AU2013204727 A AU 2013204727A AU 2013204727 A1 AU2013204727 A1 AU 2013204727A1
- Authority
- AU
- Australia
- Prior art keywords
- cobicistat
- tenofovir alafenamide
- pharmaceutically acceptable
- acceptable salt
- alafenamide hemifumarate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 230000001225 therapeutic effect Effects 0.000 title claims description 64
- 150000001875 compounds Chemical class 0.000 title description 55
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- 229960002402 cobicistat Drugs 0.000 claims abstract description 471
- LDEKQSIMHVQZJK-CAQYMETFSA-N tenofovir alafenamide Chemical compound O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1 LDEKQSIMHVQZJK-CAQYMETFSA-N 0.000 claims abstract description 378
- 229960004946 tenofovir alafenamide Drugs 0.000 claims abstract description 355
- SVUJNSGGPUCLQZ-FQQAACOVSA-N tenofovir alafenamide fumarate Chemical compound OC(=O)\C=C\C(O)=O.O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1.O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1 SVUJNSGGPUCLQZ-FQQAACOVSA-N 0.000 claims abstract description 325
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| PCT/US2013/024451 WO2013116730A1 (en) | 2012-02-03 | 2013-02-01 | Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections |
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| EA019893B1 (ru) | 2007-02-23 | 2014-07-30 | Джилид Сайэнс, Инк. | Фармацевтическая композиция и способ лечения вич-инфекции |
| KR101687841B1 (ko) | 2008-12-09 | 2016-12-19 | 길리애드 사이언시즈, 인코포레이티드 | 톨-유사 수용체의 조절제 |
| AR087546A1 (es) | 2011-08-16 | 2014-04-03 | Gilead Sciences Inc | Hemifumarato de tenofovir alafenamida |
| CN107312039B (zh) | 2012-08-30 | 2019-06-25 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药的制备方法 |
| EP3038607A2 (en) * | 2013-08-29 | 2016-07-06 | Teva Pharmaceutical Industries Ltd. | Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir and a monolithic tablet comprising darunavir and ritonavir |
| WO2015079455A2 (en) * | 2013-11-27 | 2015-06-04 | Laurus Labs Private Limited | A recycling process for preparing tenofovir alafenamide diastereomers |
| US9463194B2 (en) | 2014-02-05 | 2016-10-11 | Gilead Sciences, Inc. | Methods of treating patients co-infected with HIV and tuberculosis |
| TW201622731A (zh) * | 2014-04-08 | 2016-07-01 | 泰瓦藥品工業有限公司 | 包含恩曲他濱（Ｅｍｔｒｉｃｉｔａｂｉｎｅ）、替諾福韋（Ｔｅｎｏｆｏｖｉｒ）、地瑞那韋（Ｄａｒｕｎａｖｉｒ）及利托那韋（Ｒｉｔｏｎａｖｉｒ）之單位劑型以及包含地瑞那韋及利托那韋之單層錠劑 |
| CN105531281B (zh) * | 2014-04-21 | 2017-12-15 | 四川海思科制药有限公司 | 一种核苷类似物及其中间体的制备方法 |
| US10076512B2 (en) | 2014-05-01 | 2018-09-18 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| US11311519B2 (en) | 2014-05-01 | 2022-04-26 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| CA2954056C (en) * | 2014-07-11 | 2020-04-28 | Gilead Sciences, Inc. | Modulators of toll-like receptors for the treatment of hiv |
| JP2017526730A (ja) | 2014-09-16 | 2017-09-14 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔｏｌｌ様受容体モジュレーターの固体形態 |
| CN105237571B (zh) * | 2014-11-28 | 2018-03-09 | 成都苑东生物制药股份有限公司 | 9‑[(r)‑2‑[[(s)‑[[(s)‑1‑(异丙氧基羰基)乙基]氨基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤的盐 |
| US20180338993A1 (en) * | 2014-12-04 | 2018-11-29 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| KR20230130175A (ko) | 2014-12-26 | 2023-09-11 | 에모리 유니버시티 | Ｎ4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도 |
| EP3240793A1 (en) * | 2015-01-03 | 2017-11-08 | Mylan Laboratories Ltd. | Processes for the preparation of amorphous tenofovir alafenamide hemifumarate and a premix thereof |
| DK3285768T3 (da) | 2015-04-21 | 2021-01-25 | Eiger Biopharmaceuticals Inc | Farmaceutiske sammensætninger omfattende lonafarnib og ritonavir |
| CN104817593B (zh) * | 2015-04-27 | 2016-11-16 | 广州同隽医药科技有限公司 | 半富马酸替诺福韦艾拉酚胺关键中间体的合成工艺 |
| BR112017027843A2 (pt) * | 2015-06-30 | 2018-09-04 | Gilead Sciences, Inc. | formulações farmacêuticas compreendendo tenofovir e emtricitabina |
| CA2921336A1 (en) * | 2015-06-30 | 2016-12-30 | Gilead Sciences, Inc. | Pharmaceutical formulations |
| US9598459B2 (en) | 2015-08-03 | 2017-03-21 | Pop Test Oncology Llc | Pharmaceutical compositions and methods |
| CN105153231A (zh) * | 2015-08-28 | 2015-12-16 | 浙江车头制药股份有限公司 | 一种一苯基pmpa的制备方法 |
| BR102016026127A2 (pt) * | 2015-11-09 | 2017-05-16 | Gilead Sciences Inc | composições terapêuticas para o tratamento do vírus da imunodeficiência humana |
| AU2017218800B2 (en) * | 2016-02-12 | 2022-09-22 | Cipla Limited | Pharmaceutical compositions comprising an anti-retroviral drug and a pharmacokinetic enhancer |
| CN107179355B (zh) * | 2016-03-11 | 2021-08-10 | 广东东阳光药业有限公司 | 一种分离检测替诺福韦艾拉酚胺及其有关物质的方法 |
| EP3503895B1 (en) * | 2016-08-25 | 2021-09-15 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| CN108070003A (zh) * | 2016-12-02 | 2018-05-25 | 上海博志研新药物技术有限公司 | 替诺福韦艾拉酚胺半反丁烯二酸盐晶型及制备方法和应用 |
| RU2659388C1 (ru) | 2017-02-28 | 2018-07-02 | Васильевич Иващенко Александр | Нуклеотиды, включающие N-[(S)-1-циклобутоксикарбонил]фосфорамидатный фрагмент, их аналоги и их применение |
| RU2647576C1 (ru) * | 2017-02-28 | 2018-03-16 | Васильевич Иващенко Александр | Циклобутил (S)-2-[[[(R)-2-(6-аминопурин-9-ил)-1-метил-этокси]метил-фенокси-фосфорил]амино]-пропаноаты, способ их получения и применения |
| CN106928277A (zh) * | 2017-03-16 | 2017-07-07 | 江苏诚信药业有限公司 | 一种替诺福韦艾拉酚胺合成的工艺方法 |
| EP3600332B1 (en) | 2017-03-20 | 2023-12-13 | The United States of America, as represented by the Secretary, Department of Health and Human Services | Hiv post-exposure prophylaxis |
| US11234981B2 (en) * | 2017-04-18 | 2022-02-01 | Cipla Limited | Combination therapy for use in treating retroviral infections |
| RU2659693C1 (ru) * | 2017-06-30 | 2018-07-03 | Общество с ограниченной ответственностью "Изварино Фарма" | Фармацевтическая композиция, обладающая активностью против ВИЧ-инфекции |
| EP3700573A1 (en) * | 2017-10-24 | 2020-09-02 | Gilead Sciences, Inc. | Methods of treating patients co-infected with a virus and tuberculosis |
| AU2018378832B9 (en) | 2017-12-07 | 2021-05-27 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| CN110305163A (zh) * | 2018-03-27 | 2019-10-08 | 北京济美堂医药研究有限公司 | 替诺福韦艾拉酚胺半富马酸盐的制备方法 |
| CN108484672A (zh) * | 2018-05-23 | 2018-09-04 | 中国药科大学制药有限公司 | 磷丙替诺福韦的手性拆分方法 |
| CN109081853A (zh) * | 2018-09-03 | 2018-12-25 | 南京正大天晴制药有限公司 | 一种磷丙替诺福韦有关物质的制备方法 |
| US20220265689A1 (en) | 2019-07-19 | 2022-08-25 | THE UNITED STATES OF AMERICA , as represented by the Secretary, Department of Health and Human | Hiv pre-exposure prophylaxis |
| CN111606949A (zh) * | 2020-03-13 | 2020-09-01 | 浙江车头制药股份有限公司 | 一种磷丙替诺福韦杂质的制备方法 |
| CN111303209A (zh) * | 2020-03-21 | 2020-06-19 | 石家庄龙泽制药股份有限公司 | 一种丙酚替诺福韦降解杂质的制备方法 |
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| ES2536972T5 (es) | 2000-07-21 | 2022-04-06 | Gilead Sciences Inc | Profármacos de análogos de nucleótidos de fosfonato y métodos para seleccionar y preparar los mismos |
| DE10153078A1 (de) | 2001-10-30 | 2003-05-22 | Degussa | Verwendung von Granulaten auf Basis von pyrogen hergestelltem Siliciumdioxid in pharmazeutischen Zusammensetzungen |
| AU2004206821C1 (en) | 2003-01-14 | 2009-10-01 | Gilead Sciences, Inc. | Compositions and methods for combination antiviral therapy |
| EA019893B1 (ru) * | 2007-02-23 | 2014-07-30 | Джилид Сайэнс, Инк. | Фармацевтическая композиция и способ лечения вич-инфекции |
| KR20100041798A (ko) | 2007-06-29 | 2010-04-22 | 한국화학연구원 | 신규 ｈｉｖ 역전사효소 억제제 |
| KR101738325B1 (ko) * | 2009-02-06 | 2017-05-19 | 길리애드 사이언시즈, 인코포레이티드 | 조합 요법용 정제 |
| AR087546A1 (es) * | 2011-08-16 | 2014-04-03 | Gilead Sciences Inc | Hemifumarato de tenofovir alafenamida |
-
2013
- 2013-02-01 CN CN201380007670.XA patent/CN104105484A/zh active Pending
- 2013-02-01 US US14/376,116 patent/US20150105350A1/en not_active Abandoned
- 2013-02-01 MD MDA20140091A patent/MD20140091A2/ru not_active Application Discontinuation
- 2013-02-01 WO PCT/US2013/024451 patent/WO2013116730A1/en active Application Filing
- 2013-02-01 BR BR112014018918A patent/BR112014018918A8/pt not_active IP Right Cessation
- 2013-02-01 JP JP2014555783A patent/JP6059255B2/ja active Active
- 2013-02-01 EP EP13704863.3A patent/EP2809323A1/en not_active Withdrawn
- 2013-02-01 MX MX2014009172A patent/MX2014009172A/es unknown
- 2013-02-01 WO PCT/US2013/024438 patent/WO2013116720A1/en active Application Filing
- 2013-02-01 EA EA201491287A patent/EA026138B1/ru unknown
- 2013-02-01 NZ NZ629896A patent/NZ629896A/en unknown
- 2013-02-01 CA CA 2863662 patent/CA2863662A1/en not_active Abandoned
- 2013-02-01 AU AU2013204731A patent/AU2013204731C1/en active Active
- 2013-02-01 AU AU2013204727A patent/AU2013204727A1/en not_active Abandoned
- 2013-02-01 KR KR20147024291A patent/KR20140119177A/ko not_active Application Discontinuation
-
2014
- 2014-07-30 IL IL233874A patent/IL233874A0/en unknown
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2015
- 2015-04-07 HK HK15103394.9A patent/HK1202801A1/xx unknown
- 2015-05-27 HK HK15105031.3A patent/HK1204914A1/xx unknown
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2016
- 2016-06-02 AU AU2016203666A patent/AU2016203666A1/en not_active Abandoned
- 2016-10-03 US US15/284,105 patent/US20170056423A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20150105350A1 (en) | 2015-04-16 |
| JP2015505565A (ja) | 2015-02-23 |
| MD20140091A2 (ru) | 2015-01-31 |
| AU2013204731B2 (en) | 2016-03-03 |
| BR112014018918A8 (pt) | 2017-07-11 |
| AU2013204731A1 (en) | 2013-08-22 |
| KR20140119177A (ko) | 2014-10-08 |
| MX2014009172A (es) | 2014-08-27 |
| JP6059255B2 (ja) | 2017-01-11 |
| AU2013204731C1 (en) | 2017-08-31 |
| HK1202801A1 (en) | 2015-10-09 |
| EA026138B1 (ru) | 2017-03-31 |
| AU2016203666A1 (en) | 2016-06-23 |
| NZ629896A (en) | 2016-03-31 |
| EA201491287A1 (ru) | 2015-04-30 |
| EP2809323A1 (en) | 2014-12-10 |
| WO2013116730A1 (en) | 2013-08-08 |
| IL233874A0 (en) | 2014-09-30 |
| CN104105484A (zh) | 2014-10-15 |
| WO2013116720A1 (en) | 2013-08-08 |
| CA2863662A1 (en) | 2013-08-08 |
| US20170056423A1 (en) | 2017-03-02 |
| BR112014018918A2 (ru) | 2017-06-20 |
| HK1204914A1 (en) | 2015-12-11 |
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